Benzimidazole compounds containing aromatic substituents, processes for their preparation and uses thereof

By designing benzimidazole compounds containing aromatic substituents, the problem of EET accumulation caused by the high catalytic activity of sEH was solved, resulting in a highly efficient soluble epoxide hydrolase inhibitor that can treat a variety of diseases, including hypertension, cardiovascular disease and inflammation, and can also treat central nervous system disorders.

CN117466863BActive Publication Date: 2026-03-24OPEN SOURCE THERAPEUTICS
6 Cites 0 Cited by

Patent Information

Application Number
CN202210857338.3
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2022-07-20
Publication Date
2026-03-24
Estimated Expiration
2042-07-20

AI Technical Summary

Technical Problem

The high catalytic activity of soluble epoxide hydrolase (sEH) in the prior art prevents the effective accumulation of the bioactive lipid signaling molecule EET in vivo, thus hindering the effective treatment of sEH-mediated diseases such as hypertension, cardiovascular disease, and inflammation.

Method used

To develop a benzimidazole compound containing aromatic substituents, in which the benzene ring of the benzimidazole structure is directly linked to a first aromatic substituent and the imidazole ring is directly linked to a second aromatic substituent, forming a soluble epoxide hydrolase inhibitor with high inhibitory activity.

Benefits of technology

This compound exhibits extremely high inhibitory activity, with IC50 values ​​in the nanomolar range or even lower. It can effectively increase EET levels, treat sEH-mediated diseases, including hypertension, cardiovascular disease, and inflammation, and can cross the blood-brain barrier to treat central nervous system disorders.

✦ Generated by Eureka AI based on patent content.
Patent Text Reader

Abstract

The present application relates to an aromatic-substituted benzimidazole compound, a cis-trans isomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof. The present application also relates to a method for preparing an aromatic-substituted benzimidazole compound, and the use of the aromatic-substituted benzimidazole compound as a soluble epoxide hydrolase inhibitor. The aromatic-substituted benzimidazole compounds described herein exhibit extremely high inhibitory activity against soluble epoxide hydrolase, with IC 50 values in the nanomolar range or even lower.
Need to check novelty before this filing date? Find Prior Art